Benzimidamides compounds comprising an oxaborinin ring
AssigneeInstitut National De La Sante Et De La Recherche Medicale (Inserm)
InventorsJohn Liddle, Ann Louise Walker, Gemma Victoria White, Alexis Denis, Nerina Dodic, Marie-Hélène Fouchet, Anne Bouillot
Life of this patent
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Abstract
The invention relates to 4-(1-hydroxy-3,4-dihydro-1H-benzo[c][1,2]oxaborinin-3-yl)benzimidamide derivatives and their use in treating diseases and conditions of the skin (for example, Netherton syndrome, rosacea, atopic dermatitis, psoriasis and itch) caused by abnormally high levels of protease activity (particularly of serine proteases such as kallikreins). In addition, the invention relates to compositions containing the derivatives and processes for their preparation.
Claims19
A method of treating a disease or condition mediated by a kallikrein 5 (KLK-5) receptor in a patient comprising at least a step of administering to said patient an effective amount of a compound of formula (I):
- or a pharmaceutically acceptable salt thereof, wherein
- R1 is H, R2 is CF3 and R3 is 3-pyridylmethoxy, 3-chlorobenzyloxy or H;
- R1 is Cl, R2 is F and R3 is 3-pyridylmethoxy;
- or
- R1 is H, R2 is H and R3 is 3-pyridylmethoxy, wherein the disease or condition is selected from the group consisting of:
- Netherton syndrome, rosacea, atopic dermatitis, psoriasis and itch.
A method for preparing a pharmaceutical composition comprising at least a step of mixing a compound of formula (I):
- or a pharmaceutically salt thereof, wherein
- R1 is H, R2 is CF3 and R3 is 3-pyridylmethoxy, 3-chlorobenzyloxy or H;
- R1 is Cl, R2 is F and R3 is 3-pyridylmethoxy;
- or
- R1 is H, R2 is H and R3 is 3-pyridylmethoxy,
- with one or more pharmaceutically acceptable excipients.
Dependencies are inferred from the claim text.